Effects of cytochrome P450 (CYP3A4 and CYP2C19) inhibition and induction on the exposure of selumetinib, a MEK1/2 inhibitor, in healthy subjects: results from two clinical trials

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• 作者：Angela W. Dymond ; Karen So ; Paul Martin…
• 关键词：Selumetinib ; Exposure ; Cytochrome P450 ; Inhibition ; Induction ; Pharmacokinetic profile
• 刊名：European Journal of Clinical Pharmacology
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：73
• 期：2
• 页码：175-184
• 全文大小：486KB
• 刊物类别：Biomedical and Life Sciences
• 刊物主题：Pharmacology/Toxicology;
• 出版者：Springer Berlin Heidelberg
• ISSN：1432-1041
• 卷排序：73

文摘

PurposeTwo phase I, open-label trials in healthy subjects assessed whether co-administration with CYP3A4/CYP2C19 inhibitors, itraconazole/fluconazole (study A), or CYP3A4 inducer, rifampicin (study B), affects the exposure, safety/tolerability and pharmacokinetics of selumetinib and its metabolite N-desmethyl selumetinib.